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C-terminal modified (n-substituted)-2-indolyl dipeptides as inhibitors of the ice/ced-3 family of cysteine proteases and for treatments of inflammatory, autoimmune, neurodegenerative disorders and in the prevention of ischemic injury
C-terminal modified (n-substituted)-2-indolyl dipeptides as inhibitors of the ice/ced-3 family of cysteine proteases and for treatments of inflammatory, autoimmune, neurodegenerative disorders and in the prevention of ischemic injury
The application is directed to (N-substituted)indole ICE/ced-3-inhibitor compounds of the formula I where n is 1 or 2; R1 is alkyl, cycloalkyl, optionally substituted phenyl, phenylalkyl, heteroaryl and (CH2)mCO2R; R2 is R1, H or Cl; R3 is H, alkyl, cycloalkyl, phenylalkyl, or substituted phenyl alkyl, and X and Y each are H, halo, trihalomethyl, amino, substituted amino, carboxy, hydroxy, alkoxy, alkylthio, optionally substituted alkyl, optionally substituted cycloalkyl, and optionally substituted phenyl. Also included are pharmaceutical compositions of such indole compounds, and the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, and for the prevention of ischemic injury.
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机译:本申请涉及式I的(N-取代的)吲哚ICE / ced-3-抑制剂,其中n为1或2; R1为烷基,环烷基,任选取代的苯基,苯基烷基,杂芳基和(CH2)mCO2R; R2为R1,H或Cl; R 3是H,烷基,环烷基,苯基烷基或取代的苯基烷基,并且X和Y分别是H,卤素,三卤甲基,氨基,取代的氨基,羧基,羟基,烷氧基,烷硫基,任选取代的烷基,任选取代的环烷基,和任选取代的苯基。还包括此类吲哚化合物的药物组合物,以及此类组合物在治疗患有炎性,自身免疫和神经退行性疾病的患者中以及在预防缺血性损伤中的用途。
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